Chemical Structure : TRAP-1
CAS No.:
TRAP-1
(TRAP1)
Catalog No.: PC-23521Not For Human Use, Lab Use Only.
TRAP-1 is a small molecule chemical inducer of proximity that activates mutant p53, engages mutant p53Y220C and BRD4 in a ternary complex, which potently activates mutant p53 and triggers robust p53 target gene transcription.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TRAP-1 is a small molecule chemical inducer of proximity that activates mutant p53, engages mutant p53Y220C and BRD4 in a ternary complex, which potently activates mutant p53 and triggers robust p53 target gene transcription.
TRAP-1 induces a stable interaction between p53Y220C and BRD4. exhibited antiproliferative activity in BxPC-3 (p53Y220C) cells with submicromolar IC50 values (BxPC-3. IC50=0.53 uM).
TRAP-1 induces a mutant-specific ternary complex formation, resulting in a potent and selective antiproliferative effect against p53Y220C bearing cancer cells.
TRAP-1 induces rapid upregulation of p21 and other p53 target genes and inhibits the growth of p53Y220C-expressing cell lines.
Physicochemical Properties
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M.Wt
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1108.71
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Formula
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C57H66ClF3N11O3PS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-1-(4-((1-(2-(4-((2-(3-((4-(dimethylphosphoryl)phenyl)amino)prop-1-yn-1-yl)-1-(2,2,2-trifluoroethyl)-1H-indol-4-yl)amino)piperidin-1-yl)acetyl)piperidin-4-yl)methyl)piperazin-1-yl)ethan-1-one
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References
1. Zhu X, et al. bioRxiv [Preprint]. 2024 Oct 28:2024.10.23.619961.
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